Assay Detail

CHEMBL989223

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Binding

Inhibition of mouse c-Met by HTRF assay

ChEMBL ↗

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Target

Hepatocyte growth factor receptor (CHEMBL5585) ↗

Open DB target context

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Hepatocyte growth factor receptor (CHEMBL5585) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Hepatocyte growth factor receptor

CHEMBL5585

Anchored from Assay target.

Protein identity Hepatocyte growth factor receptor

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Mus musculus
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Hepatocyte growth factor receptor (CHEMBL5585) ↗

Type	SINGLE PROTEIN
Organism	Mus musculus

Publication

Discovery of a potent, selective, and orally bioavailable c-Met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458).

Liu L, Siegmund A, Xi N, Kaplan-Lefko P, Rex K, Chen A, Lin J, Moriguchi J, Berry L, Huang L, Teffera Y, Yang Y, Zhang Y, Bellon SF, Lee M, Shimanovich R, Bak A, Dominguez C, Norman MH, Harmange JC, Dussault I, Kim TS.
J Med Chem (2008) 51 : 3688 -3691
PubMed 18553959 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Ki	1	8.70	8.70

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL460472	—	—	1	8.70

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL460472	—	Ki	=	2.0	nM	8.70